Effect-time-relation of the H1-receptor antagonist dimethindene maleate following intravenous injection.

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Rehn D, Geissler H, Schonbrunn U, Lukas H, Hennings G

Effect-time-relation of the H1-receptor antagonist dimethindene maleate following intravenous injection.

Agents Actions. 1990 Apr;30(1-2):178-81. doi: 10.1007/BF01969031.

PubMed ID

1973583 [ View in PubMed

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Abstract

We have investigated the time-course of the weal and flare inhibiting activity of dimethindene maleate in man and compared the resulting effect-kinetic data with those from pharmacokinetic investigations. The study was carried out in a double blind, placebo controlled cross-over design with randomly assigned healthy volunteers. Dimethindene maleate (4 mg) was intravenously injected, followed by intracutaneous histamine provocations (-1, 2, 5, 14, 17, 20, 23, 26, and 29 h). The two cross-over periods were separated by a wash-out phase of 17 h. Flare and weal areas were documented 5, 10, 20, and 30 min after provocation with histamine. A strong inhibition of the development of flares and weals was observed and was more pronounced in flares than in weals. With regard to the time course of the inhibiting effect, its maxima both for flares and weals were observed at a provocation time of 2 h. The mean residence time of the inhibiting effect was calculated to be ca. 13 h for flares and ca. 15 h for weals. These values are nearly 2-3 times as high as the mean residence time of 6 h calculated from blood level data. Blood- and effect-levels are thus non-linearly related.

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Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dimetindene	Histamine H1 receptor	Protein	Humans	Yes	Antagonist	Details